Abstract: Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds whereinA is.dbd.CR.sup.6 --;R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl;R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group;R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; andR.sup.6 is halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl),as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

Abstract: Novel pyridyloxy-acrylic acid esters of the formula ##STR1## in which Ar represents optionally substituted aryl or represents optionally substituted heteroaryl,a process for preparing the novel compounds and their use as agents for combating pests.Novel intermediates, processes for their preparation and their use for the synthesis of pyridyloxy-acrylic acid esters.

Abstract: Heterocyclic compounds of the formula: ##STR1## and a cardiotonic agent containing the same which have an excellent positive inotropic effect and which suppress increase of heart rate.

Abstract: This invention provides thiadiazinone derivatives represented by the following formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or C.sub.1 -C.sub.5 alkyl, R.sup.2 represents a 5- or 6-membered heterocyclic ring having (a) 1-3 nitrogen atoms, (b) a oxygen atom, (c) one sulfur atom, (d) 1-3 nitrogen atoms and one oxygen atom, or (e) 1-3 nitrogen atoms and one sulfur atom each of which rings may optionally be substituted by at least one substituent selected from the group consisting of C.sub.1 -C.sub.5 alkyl, cyano, hydroxy, C.sub.1 -C.sub.5 alkoxy, amino, C.sub.1 -C.sub.5 alkylamino, C.sub.2 -C.sub.6 dialkylamino, C.sub.2 -C.sub.5 acylamino, carboxyl, C.sub.2 -C.sub.5 alkoxycarbonyl and carbamoyl; or a pharmaceutically acceptable salt thereof. The compounds according to the present invention have an excellent cardiotonic activity, and are useful as active ingredients of a cardiotonic drug.

Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R.sup.1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.

Abstract: Substantially dust-free granules of tetrahydro-3,5-dimethyl-1,3,5-thiadiazine-2-thione (I) are prepared by reacting methylamine (II) with carbon disulfide (III) and formaldehyde (IV) or by reacting the methylammonium salt of N-methyldithiocarbamic acid (V) with formaldehyde (IV) by a process in which the reaction is carried out in the presence of at least one diaminoalkylene of the formula VIR.sup.1 -NH-A-NH-R.sup.2 VIwhere R.sup.1 and R.sup.2 independently of one another are each hydrogen or alkyl and A is an unsubstituted or substituted 1,2-ethylene, 1,3-propylene or 1,4-butylene bridge.

Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.

Abstract: The present invention relates to a novel heterocyclic compound having excellent positive inotropic effect as cardiotonic agent and suppressing increase of heart rate and a cardiotonic agent containing the novel heterocyclic compound as active component.

Abstract: The present invention relates to thiadiazinones of the formula I ##STR1## having a phosphodiesterase-inhibiting action and which are suitable for combating cardiovascular and asthmatic disorders.

Abstract: A compound having the formula ##STR1## wherein A is CR.sub.7 ; and R.sup.1 through R.sup.7 are substituents such as hydrogen, halogen, branched and straight chain hydrocarbons, cyclic hydrocarbons, aromatics, and sulfur and nitrogen containing functional groups. Further, R.sup.5 and R.sup.6 may be taken together with the atom to which they are attached to form a group ##STR2## in which R.sup.9 and R.sup.10 are further functional groups. The compounds are useful in herbicidal compositions, particularly in combination with carriers and surfactants. A process for making this compound is also presented.

Abstract: The invention relates to thiadiazinecarboxamide derivatives of the general formula I ##STR1## to processes for their preparation, and to pharmaceuticals comprising them.

Abstract: Benzimidazole compounds of the formula I ##STR1## and salts thereof, exhibit antagonistic properties toward angiotensin II and can be used for the treatment of hypertension, aldosteronism, cardiac insufficiency and an increased intraocular pressure, as well as disturbances of the central nervous system.

Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.

Abstract: Thiadiazinones of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n have the meaning given in claim 1, show antiarrhythmic action and are suitable for the control of cardiovascular disorders.

Abstract: The present invention relates to an uracil derivative represented by the formula (1): ##STR1## in which R.sup.1 represents hydrogen, alkyl or haloalkyl; R.sup.2 represents haloalkyl; R.sup.3 represents hydrogen, alkyl, haloalkyl, hydroxymethyl, halogen or nitro; R.sup.4 represents hydrogen or halogen; R.sup.5 represents hydrogen, halogen, nitro or cyano; X represents oxygen or sulfur: provided that the case where both of Da and Db represent hydrogen is excluded and a herbicide containing the same. The compound can be safely applied to important crops and shows high effect against many weeds in a low amount.

Abstract: Methods are provided whereby an N-C-N compound is regenerated from a product of a sulfur scavenging reaction, in which said N-C-N compound removes a sulfur atom from a sulfur compound, to form the original N-C-N compound. The N-C-N compound is represented by the formula (I): ##STR1## The product includes a hetero compound having sulfur, carbon and nitrogen atoms in its backbone. In one embodiment, the product is mixed with (1) a nitrogen compound represented by the formula (II): ##STR2## and (2) an alkaline compound selected from alkali metal, alkaline earth metal and transition metal compounds, to form a solution, slurry or dispersion. The hetero compound is reacted with the nitrogen compound in the presence of the alkaline compound, such that a sulfur atom of the hetero compound is replaced by a nitrogen atom of the nitrogen compound. If necessary, the pH of the solution may be adjusted to about 8 to about 13 to facilitate the reaction. In alternative embodiments, the product also includes an amine complex.

Abstract: A solvent soluble heterocyclic o-hydroxy thione carrying a lipophilic group and the process for the selective extraction of gallium, and certain other related metals, especially from solutions containing excess aluminium.

Abstract: Compounds of formula I ##STR1## in which R.sup.1 and R.sup.2 are each independently of one another H or A,R.sup.3 is H, OA or O--C.sub.m H.sub.2m+1-n X.sub.n,R.sup.4 is --O--C.sub.m H.sub.2m+1-n X.sub.n,X is F or Cl,A is alkyl having 1-6 C atoms,m is 1, 2, 3, 4, 5 or 6 andn is 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13, and their salts have positive ionitropic activity and vasodilating action, and promote circulation. In addition, the compounds can be employed for the treatment of asthmatic disease and memory disorders, and have anti-depressive and anti-inflammatory properties.

Abstract: The invention concerns an aryl derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a heterocyclic moiety, and X.sup.1 is oxy, thio, sulphinyl, sulphonyl, difluoromethylene, imino, (1-4C)alkylimino or optionally substituted (1-4C)alkylene, or X.sup.1 is a group of the formula--X.sup.4 --CR.sub.2 -- or --CR.sub.2 --X.sup.4 --whereinX.sup.4 is oxy, thio, sulphinyl, sulphonyl or carbonyl and each R is hydrogen, methyl or ethyl;each of Ar.sup.2 and Ar.sup.3 is optionally substituted phenylene;X.sup.2 is oxy, thio, sulphinyl or sulphonyl;R.sup.1 is (1-4C)alkyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X.sup.3 --A.sup.2 -- which together with the carbon atom to which A.sup.1 and A.sup.2 are attached define a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X.sup.

Abstract: This invention relates to N-phenylpyridone derivatives which have inotropic, vasodilator and bronchodilator activity. A compound of the invention is 5-methyl-6-[4-(4-oxo-1,4-dihydropyridin-1-yl)phenyl]-4,5-dihydro-3(2H)pyri dazinone.

Abstract: A process for the preparation of 1,3-disubstituted 2-nitroguanidines of the formula I ##STR1## in which R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or a radical --CH.sub.2 B; A is an unsubstituted or mono- to tetrasubstituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical, which may contain one or two substituents from the group comprising C.sub.1 -C.sub.3 haloalkyl having 1 to 7 halogen atoms, cyclopropyl, halocyclopropyl having 1 to 3 halogen atoms, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl, C.sub.2 -C.sub.3 haloalkenyl and C.sub.2 -C.sub.3 haloalkynyl having 1 to 4 halogen atoms, C.sub.1 -C.sub.3 haloalkoxy having 1 to 7 halogen atoms, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloalkylthio having 1 to 7 halogen atoms, allyloxy, propargyloxy, allylthio, propargylthio, haloallyloxy, haloallylthio, cyano and nitro and one to four substituents from the group comprising C.sub.1 -C.sub.3 alkyl, C.sub.

Abstract: The invention relates to a process for the resolution of enantiomers of 5-heteroaryl-1,3,4-thiadiazinones of formula I by the kinetic resolution of racemates, characterized in that racemic I is dissolved in an inert solvent or solvent mixture and acylated with a chiral acid chloride. The resulting mixture of diastereoisomers is reacted with an amine or alcohol, thereby achieving a complete resolution of one of the diastereoisomers and a very slight or partial resolution of the other diastereoisomer into the enantiomers on which they are based, the resolution products are then separated off and the remaining pure diastereoisomer is converted to the corresponding pure enantiomer by reaction with an amine or an alcohol.

Abstract: A class of substituted cyclic sulphamide derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.

Abstract: Triphendioxazine dyes suitable for dyeing or printing hydroxyl- or amido-containing substrates have the formula ##STR1## where n is 0 or 1,m is 1 or 2,R.sup.1 and R.sup.2 are each independently of the other hydrogen, chlorine, bromine, hydroxysulfonyl, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, substituted or unsubstituted phenyl or substituted or unsubstituted phenoxy,R.sup.3 is halogen, carboxyl, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, vinylsulfonyl or the radical --SO.sub.2 --CH.sub.2 CH.sub.2 --Z, where Z is a leaving group, andQ.sup.1 and Q.sup.2 are each independently of the other a radical of the formula ##STR2## where R.sup.4 and R.sup.5 are each independently of the other hydrogen, C.sub.1 -C.sub.4 -alkyl or phenyl,R.sup.6 is hydrogen or a fiber-reactive radical,L.sup.1 and L.sup.2 are each independently of the other substituted or unsubstituted C.sub.2 -C.sub.8 -alkylene or phenylene,X is a chemical bond, oxygen, sulfur, imino, C.sub.1 -C.sub.

Abstract: New heterocyclic compounds of formula I ##STR1## In which Het means one of following groups; ##STR2## wherein R.sub.11, R.sub.13 and R.sub.14 mean independently hydrogen, hydroxymethyl or lower alkyl group, Z means S, O or NH; A means valency bond, --CH.dbd.CH--, or --CH.sub.2 --CH.sub.2 --group; R.sub.1 and R.sub.2 independently mean nitro, cyano, halogen, amino, carboxamido, aryl, aroyl, pyridyl, alkoxycarbonyl, acyl or one of following groups; ##STR3## wherein R.sub.6 means hydrogen or lower alkyl group, R.sub.8 means lower alkyl, R.sub.7 means cyano or COOR.sub.10, wherein R.sub.10 means hydrgen or lower alkyl or R.sub.1 and R.sub.2 together form a susbtituted or unsubstituted 5 or 6 membered ring which may contain 1 to 2 heteroatom N; R.sub.3, R.sub.4, and R.sub.5 means independently hydrogen, hydroxy or lower alkyl group; Y means N or CH. The compounds may be used in the treatment of congestive heart failure.

Abstract: Novel .beta.-form crystals of 6-(3,6-dihydro-2-oxo-2H-1,3,4-thiadiazin-5-yl)-3,4-dihydro-2(1H)-quinolino ne useful as cardiotonics.

Abstract: Mono-acylated hydrazines are prepared in high yield by reaction of a hydrazine salt with an azole derivative of acyl halide in the presence of a strong base. Useful hydrazine salts include those of the formula RNHNH.sub.2 .multidot.HX, where R is alkyl, aryl, aralkyl, acyl, aroyl, heterocyclic or heteroaryl, and HX is a mineral or organic acid. Useful azole derivatives include those of the formula R'CO--A, where R' is alkyl, aryl, aralkyl, heterocyclic or heteroaryl and A is an azole radical such as pyrrole, imidazole, pyrazole, triazole, tetrazole, indole or benzimidazole.

Abstract: What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.

Abstract: A sulfamidosulfonamide derivative of the formula (1) and an agriculturally suitable salt thereof: ##STR1## wherein Q is ##STR2## X is an oxygen atom or a sulfur atom; and G is ##STR3## which are useful as herbicide.

Abstract: Thiadiazinones of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meaning given in claim 1, show positively inotropic and vasodilating action and are suitable for combating cardiovascular diseases.

Abstract: There is disclosed a method for producing 2,6-bis(disubstituted amino)-1,3,5-thiadiazine-4-one compounds represented by formula (I). The method comprises reacting an N,N-disubstituted cyanamide represented by formula (II) with carbonyl sulfide represented by formula (III) under a high pressure. Formula (I) ##STR1## wherein R.sub.1 and R.sub.2 each represent an alkyl group or R.sub.1 and R.sub.2 may bond together to form a ring, Formula (II) ##STR2## wherein R.sub.1 and R.sub.2 each have the same meanings as in formula (I), Formula (III)S.dbd.C.dbd.O.

Abstract: New heterocyclic compounds of formula I ##STR1## in which Het means one of following groups; ##STR2## wherein R.sub.11, R.sub.13 and R.sub.14 mean independently hydrogen, hydroxymethyl or lower alkyl group, Z means S, O or NH; A means valency bond, --CH.dbd.CH--, or --CH.sub.2 --CH.sub.2 -- group; R.sub.1 and R.sub.2 independently mean nitro, cyano, halogen, amino, carboxamido, aryl, aroyl, pyridyl, alkoxycarbonyl, acyl or one of following groups; ##STR3## wherein R.sub.6 means hydrogen or lower alkyl group, R.sub.8 means lower alkyl, R.sub.7 means cyano or COOR.sub.10, wherein R.sub.10 means hydrogen or lower alkyl or R.sub.1 and R.sub.2 together form a substituted or unsubstituted 5 or 6 membered ring which may contain 1 or 2 heteroatom N; R.sub.3, R.sub.4, and R.sub.5 mean independently hydrogen, hydroxy or lower alkyl group; Y means N or CH. The compounds may be used in the treatment of congestive heart failure.

Abstract: New diazine derivatives corresponding to the general formula I ##STR1## and the physiologically acceptable salts thereof are described. The compounds according to the invention are new positive inotropic compounds having a higher and/or more selective action than compounds hitherto known and are therefore suitable for the treatment and prevention of diseases of the heart and circulation.

Abstract: Heterocyclic compounds of the formula ##STR1## are used as pigments for surface coatings and for coloring and pigmenting high molecular weight organic material.

Abstract: There is disclosed a novel thiadiazine, 2,6-bis(disubstituted amino)-4-dialkylthiocarbamoylimino-1,3,5-thiadiazine, and method for preparing same. According to the disclosure a compound useful for a medicine and agricultural chemical can be obtained efficiently by a one-step reaction using inexpensive raw materials.

Abstract: S-(N-alkoxycarbonyl, N-substituted)amino methyl isothiourea derivative, which is a useful intermediate for the production of 1,3,5-thiadiazine-4-one derivative, is disclosed. The above compound can be produced by reacting the carbamate compound of the formula(II) with the thiourea compound of the formula(III).

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, ##STR1## in which, R.sub.1 is hydrogen or lower alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.4 and R.sub.4 ' together form a group .dbd.N--Ra, or .dbd.CRaRb, where Ra is hydrogen, lower alkyl, aryl, aryloxy, lower alkylcarbonyl, arylcarbonyl, aryloxycarbonyl, lower alkoxy, lower alkoxy carbonyl, lower alkoxy carbonyl alkoxy, lower thioalkoxy, hydroxy, nitrile, heterocyclyl, or --NRcRd, where Rc is hydrogen, lower alkyl, cycloalkyl, aryl, aralkyl, lower alkylcarbonyl, arylcarbonyl, aminocarbonyl, aminothiocarbonyl, aminoiminocarbonyl, lower alkoxycarbonyl, lower alkoxythiocarbonyl, aryloxycarbonyl, thiocarbonyl, nitrile, carboxyl, heterocyclyl or heterocyclylcarbonyl, and Rd is hydrogen or lower alkyl; Rb is hydrogen, lower alkyl, aryl, lower alkylcarbonyl, lower alkoxycarbonyl, nitrile or nitro;or R.sub.4 is --NH--Ra, in which Ra is as defined above, and R.sub.4 ' is hydrogen or lower alkyl;each of R.sub.3 and R.sub.

Abstract: Pyrimidine compounds useful as plant growth regulators have the formula (I): ##STR1## wherein Y is an optionally substituted secondary or tertiary alkyl group containing from 3 to 7 carbon atoms or an optionally substituted cycloalkyl or alkylcycloalkyl group containing from 3 to 7 carbon atoms; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen or a lower alkyl group; A is an optionally substituted heterocyclic group, for example thienyl or pyridyl; n is an integer which may be from 0 to 2 and is preferably 0; and R.sup.3 is hydrogen, an alkyl group containing from 1 to 4 carbon atoms, or an alkenyl or alkynyl group containing from 2 to 4 carbon atoms.

Abstract: Novel tetrahydro-1,3,5-thiadiazin-4-ones of the following general formula (I) or their salts which are useful as an insecticidal and acaricidal agent. ##STR1## In the formula, each of R.sup.1 and R.sup.2 represents a halogen atom or a C.sub.1 -C.sub.4 alkyl group; R.sup.3 represents a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.6 cycloalkyl group, a C.sub.1 -C.sub.4 alkoxy group, an acetyl group, a phenoxy group, a halo-substituted phenoxy group, a benzyl group, a benzyloxy group, a phenylcarbonyl group, a C.sub.1 -C.sub.4 haloalkyloxy group, a C.sub.1 -C.sub.4 haloalkyloxymethyl group, a C.sub.2 -C.sub.4 haloalkenyloxy group, a C.sub.1 -C.sub.4 haloalkylthio group, a C.sub.1 -C.sub.4 haloalkylthiomethyl group, a C.sub.2 -C.sub.4 haloalkenylthio group, a C.sub.1 -C.sub.8 haloalkyl group, a C.sub.2 -C.sub.8 haloalkenyl group, a C.sub.1 -C.sub.

Abstract: There is disclosed compounds having, within their structural formulae, a trivalent moiety: ##STR1## which exhibit antiozonant activity when added to rubber compositions at antiozonant effective levels and which exhibit synergistic antiozonant activity when used with conventional antiozonants in rubber compositions. There is also disclosed novel compounds which can be used as antiozonants.

Abstract: New heterocyclic compounds of formula I ##STR1## in which Het means one of following groups; ##STR2## wherein R.sub.11, R.sub.13 and R.sub.14 mean independently hydrogen, hydroxymethyl or lower alkyl group, Z means S, O or NH; A means valency bond, --CH.dbd.CH--, or --CH.sub.2 --CH.sub.2 --group; R.sub.1 and R.sub.2 independently means nitro, cyano, halogen, amino, carboxamido, aryl, aroyl, pyridyl, alkoxycarbonyl, acyl or one of following groups; ##STR3## wherein R.sub.6 means hydrogen or lower alkyl group, R.sub.8 means lower alkyl, R.sub.7 means cyano or COOR.sub.10, wherein R.sub.10 means hydrogen or lower alkyl or R.sub.1 and R.sub.2 together form a substituted or unsubstituted 5 or 6 membered ring which may contain 1 or 2 heteroatom N; R.sub.3, R.sub.4, and R.sub.5 mean independently hydrogen, hydroxy or lower alkyl group; Y means N or CH. The compounds may be used in the treatment of congestive heart failure.

Abstract: A novel compound of the formula (I): ##STR1## wherein R.sub.1 is optionally esterified or amidated carboxyl; R.sub.2, R.sub.3 and R.sub.4 are the same or different and are hydrogen or alkyl; A is formyl, hydroxyiminomethyl or carboxyl; and X is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active component the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R.sub.1 is carboxyl, R.sub.2, R.sub.3 and R.sub.4 are hydrogen and X is formyl are also disclosed.

Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4 -12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group; R.sub.4 and R.sub.5, which may be the same or different and may be attached to the same or different carbon atoms of the isoquinoline nucleus, are each hydrogen, halogen, hydroxy, C.sub.1-6 alkyl, aryl, or R.sub.4 together with R.sub.5 form a --(CH.sub.2).sub.p -- group, where p is an integer of from 1 to 5 and one or more of the --(CH.sub.2)-- moieties is optionally substituted by a C.

Abstract: Novel 5-(3-alkyl-5-tert.butyl-4-hydroxyphenyl)-2-amino-6H-1,3,4-thiadiazines of the general formula I ##STR1## in which R.sup.1 =C.sub.1 -C.sub.4 -alkyl,R.sup.2 =H or C.sub.1 -C.sub.3 -alkylR.sup.3 and R.sup.4 =independently of one another, optionally substituted and optionally O- or S-interrupted alkyl, alkenyl or alkynyl groups, it being possible for one of the two radicals to also be H,or R.sup.3 +R.sup.4 together with the nitrogen atom to which they are bound, may denote an optionally substituted 4- to 7-membered ring which optionally contains a further heteroatom (O, S or N),and the physiologically acceptable acid-addition salts thereof. The compounds are primarily suitable for prevention and treatment of inflammatory--in particular inflammatory rheumatic--disorders and/or pain.

Abstract: A heterocyclic oxophthalazinyl acetic acid having aldose reductast inhibitory activity of the formula ##STR1## wherein X is oxygen or sulfur; Z is a covalent bond, O, S, NH or CH.sub.2 or CHR.sub.5 Z is vinyl; R.sub.1 is hydroxy, or a prodrug group; R.sub.2 is a heterocyclic group, R.sub.3 and R.sub.4 are hydrogen or the same or a different substituent, and R.sub.5 is hydrogen, methyl or trifluoromethyl. The pharmaceutically acceptable acid addition salts of the above compounds wherein R.sub.1 is di(C.sub.1 -C.sub.4)alkylamino or (C.sub.1 -C.sub.4)alkoxy substituted by N-morpholino or di(C.sub.1 -C.sub.4)alkylamino and the pharmaceutically active base addition salts of the above compounds wherein R.sub.1 is hydroxy are also aldose reductase inhibitors.

Abstract: A novel compound of the formula (I): ##STR1## wherein R.sub.1 is optionally esterified or amidated carboxyl; R.sub.2, R.sub.3 and R.sub.4 are the same or different and are hydrogen or halogen or alkyl; A is formyl, hydroxyiminomethyl or carboxyl; and A is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active compound the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R.sub.1 is carboxyl, R.sub.2, R.sub.3 and R.sub.4 are hydrogen and X is formyl are also disclosed.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, ##STR1## in which, R.sub.1 is hydrogen, lower alkyl or CH.sub.2 OR.sub.6 ;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen or lower alkyl;each of W and Z, which are different, represents --CR.sub.4 R.sub.5 -- or --(CR.sub.x R.sub.y).sub.n --, in which,R.sub.4 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy;R.sub.5 is C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy; or together R.sub.4 and R.sub.5 form a 3 to 6 membered carbocyclic ring, or a heterocyclic ring containing one or two ring oxygen, nitrogen or sulphur atoms;or R.sub.4 and R.sub.5 together form an oxo or methylene group;each of R.sub.x and R.sub.y is hydrogen or C.sub.1-3 alkyl; n is zero or 1;R.sub.6 is hydrogen, lower alkyl, lower alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heteroarylcarbonyl, optionally substituted aminocarbonyl, lower alkoxycarbonyl and aryloxycarbonyl;R.sub.

Abstract: Thiadiazinones of the formula I ##STR1## wherein A is --CHR.sup.4 --CHR.sup.5 --, --CH.sub.2 --CR.sup.4 R.sup.5 --, --CR.sup.4 R.sup.5 --CH.sub.2 --, --CHR.sup.4 --CHR.sup.5 --CH.sub.2 --, --CHR.sup.4 --CH.sub.2 --CHR.sup.5 --, --CH.sub.2 --CHR.sup.4 --CHR.sup.5 --, --CR.sup.4 R.sup.5 --CH.sub.2 CH.sub.2 --, --CH.sub.2 --CR.sup.4 R.sup.5 --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --CR.sup.4 R.sup.5 --,R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently H, C.sub.1-5 -alkyl, C.sub.2-5 -alkenyl or C.sub.2-5 -alkinyl,R.sup.3 is also C.sub.1-15 -acyl,R.sup.6 is H, alkyl, alkoxyl, OH, F, Cl, Br or I andZ is (H, H), (H, alkyl), (alkyl, alkyl) or O,the alkyl, alkenyl, alkinyl and/or alkoxy groups in each case containing up to 5 C atoms, but wherein, if A is --CH.sub.2 CH.sub.2 -- and Z is O, one of the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.6 must be other than H,and salts thereof demonstrate positive inotropic action and are suitable for combating cardiovascular diseases.

Abstract: Phosphodiesterase (type III) inhibitors having the formula: ##STR1## which are useful in stimulating cardiac activity and in treating congestive heart failure and bronchoconstriction, pharmaceutical compositions including these inhibitors, and methods of using these compounds to produce phosphodiesterase (type III) inhibition in mammals.

Abstract: Heterocyclic substituted indolinones of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl or hydroxyalkyl radical, R.sub.2 is a carboxyl group or an alkoxy-carbonyl, hydroxyalkyl or alkylcarbonyloxyalkyl radical or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a lactone having 4, 5 or 6 ring atoms, A-B is --CH.sub.2 --CH(R.sub.3)--, --CH.dbd.CR.sub.3 --, --CH.sub.2 --NH--, --NH--CH.sub.2 --, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.sub.2 --S-- or --S--CH.sub.2 -- radical, R.sub.3 being a hydrogen atom or an alkyl or hydroxyalkyl radical, or A is a valency bond and B is a methylene radical ##STR2## or an imino group ##STR3## R.sub.4, R.sub.5, and R.sub.